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Synthesis and Myelostimulatory Activity of β-Cyclodextrin Complexes of 3,7-Diazabicyclo[3.3.1]Nonan-9-One Derivatives
Pharmaceutical Chemistry Journal ( IF 0.9 ) Pub Date : 2020-09-01 , DOI: 10.1007/s11094-020-02243-6
A. E. Malmakova , V. K. Yu , T. K. Iskakova , P. Dauletbay , K. D. Praliev , L. K. Baktybaeva

Simultaneous Mannich condensation of 1-(3-methoxypropyl)piperidone-4 with paraformaldehyde and 1-(2-pyridinoethyl)amine yielded 3-(3methoxypropyl)-7-[2-(pyridin-2-yl)ethyl]-3,7-diazabicyclo[3.3.1]nonan-9-one, which was reduced to the corresponding bicyclic nonane under Huang—Minlon reaction conditions. The reaction of 3,7-diazabicyclo[3.3.1]nonan-9-one with hydroxylamine hydrochloride led to the corresponding oxime, subsequent acylation of which synthesized its O-benzoyloxime. Replacement of the morpholine or piperazine ring in 3-(3-ethoxy- or isopropoxypropyl)-7-[2-(N-morpholino- or N-piperazino) ethyl]-3,7-diazabicyclo[3.3.1]nonane by pyridine led to a loss of activity. However, 3-(3-methoxy- and isopropoxypropyl)-7-[2-(pyridin-2-yl- and N-piperazino)ethyl]-3,7-diazabicyclo[3.3.1]nonan-9-one O-benzoyloximes were myelostimulators although they differed in that the β-cyclodextrin complex of 3-(3-methoxypropyl)-7-[2-(pyridin-2-yl)ethyl]-3,7-diazabicyclo[3.3.1]nonan-9-one O-benzoyloxime stimulated both erythro- and leukopoiesis while its N-piperazine analog stimulated only leukopoiesis.

中文翻译:

3,7-二氮杂双环[3.3.1]Nonan-9-One衍生物的β-环糊精复合物的合成及骨髓刺激活性

1-(3-甲氧基丙基)哌啶酮-4与多聚甲醛和1-(2-吡啶基乙基)胺同时曼尼希缩合得到3-(3-甲氧基丙基)-7-[2-(吡啶-2-基)乙基]-3,7 -二氮杂双环[3.3.1]壬烷-9-one,在Huang-Minlon反应条件下被还原为相应的双环壬烷。3,7-二氮杂双环[3.3.1]壬烷-9-酮与盐酸羟胺反应生成相应的肟,随后酰化合成其O-苯甲酰肟。用吡啶替换 3-(3-乙氧基-或异丙氧基丙基)-7-[2-(N-吗啉代-或 N-哌嗪基)乙基]-3,7-二氮杂双环[3.3.1]壬烷中的吗啉或哌嗪环导致失去活动。然而,3-(3-甲氧基-和异丙氧基丙基)-7-[2-(吡啶-2-基-和N-哌嗪基)乙基]-3,7-二氮杂双环[3.3。
更新日期:2020-09-01
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